Pharmacokinetic drug-drug interaction between the COVID-19 3CL protease inhibitor GST-HG171 and itraconazole in healthy subjects

of GST-HG171 and ritonavir by approximately 8% and 28%, respectively, while systemic exposure (area under the plasma concentration-time curve [AUC]) was elevated by approximately 45% and 33%, respectively. There was no apparent increase in the incidence or severity of AEs during the co-administration period. In conclusion, co-administration of itraconazole, a strong CYP3A4 inhibitor, with GST-HG171/ritonavir resulted in a moderate increase in exposure of GST-HG171 and mild increase in exposure of ritonavir, and it had an acceptable safety profile and was well tolerated in this study.CLINICAL TRIALSThis study is registered with ClinicalTrials.gov as NCT06087055.

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Publication Details

Journal
Antimicrobial Agents and Chemotherapy
Published
2026-05-11
DOI
https://doi.org/10.1128/aac.00285-26
Primary Topic
Pharmacogenetics and Drug Metabolism
Type
article
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article

Pharmacokinetic drug-drug interaction between the COVID-19 3CL protease inhibitor GST-HG171 and itraconazole in healthy subjects

X.C. Li, George Zhang, Tianxiang Zhang, Wenhao Yan et al.
Antimicrobial Agents and Chemotherapy
Pharmacogenetics and Drug Metabolism
article

Pharmacokinetic drug-drug interaction between the COVID-19 3CL protease inhibitor GST-HG171 and itraconazole in healthy subjects

X.C. Li, George Zhang, Tianxiang Zhang, Wenhao Yan, Yi-Xiang Wang, John Mao, Meng Wang, Yanan Tang, Yanhua Ding, Chuanjing Li, Bing Li, Jing Lu
article en

Abstract

of GST-HG171 and ritonavir by approximately 8% and 28%, respectively, while systemic exposure (area under the plasma concentration-time curve [AUC]) was elevated by approximately 45% and 33%, respectively. There was no apparent increase in the incidence or severity of AEs during the co-administration period. In conclusion, co-administration of itraconazole, a strong CYP3A4 inhibitor, with GST-HG171/ritonavir resulted in a moderate increase in exposure of GST-HG171 and mild increase in exposure of ritonavir, and it had an acceptable safety profile and was well tolerated in this study.CLINICAL TRIALSThis study is registered with ClinicalTrials.gov as NCT06087055.

Antimicrobial Agents and Chemotherapy
Jilin University (CN), First Hospital of Jilin University (CN), Kai Biotech (South Korea) (KR)
Good health and well-being
Openalex Percentile: Top 6%
Pharmacogenetics and Drug Metabolism
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Pharmacokinetic drug-drug interaction between the COVID-19 3CL protease inhibitor GST-HG171 and itraconazole in healthy subjects — X.C. Li, George Zhang, et al. · Antimicrobial Agents and Chemotherapy (2026) | TGRS Research Map | TGRS